利用微波辅助的 S(N)Ar 反应协议合成氨基苯并噻唑-1,1-二氧化物。
Synthesis of amino-benzothiaoxazepine-1,1-dioxides utilizing a microwave-assisted, S(N)Ar protocol.
机构信息
Department of Chemistry, University of Kansas, Lawrence, United States.
出版信息
ACS Comb Sci. 2011 Nov 14;13(6):653-8. doi: 10.1021/co200076j. Epub 2011 Sep 8.
Abstract
The development of a microwave-assisted, intermolecular S(N)Ar protocol for the synthesis of a 126-member benzothiaoxazepine-1,1-dioxide library is reported. Diversification of 12 benzothiaoxazepine-1,1-dioxides was achieved in rapid fashion utilizing a variety of 2° amines and amino alcohols to generate an 80-member library. A second 48-member library was subsequently generated via a two-step alkylation, intermolecular S(N)Ar diversification protocol.
摘要
本文报道了一种微波辅助的分子间 S(N)Ar 反应方法，用于合成 126 个成员的苯并噻噁嗪-1,1-二氧化物文库。通过使用各种 2°胺和氨基醇，快速多样化了 12 个苯并噻噁嗪-1,1-二氧化物，生成了一个 80 成员的文库。随后，通过两步烷基化、分子间 S(N)Ar 多样化反应方案，生成了第二个 48 成员的文库。
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